Department of Pharmacology and Toxicology, University at Buffalo, Buffalo, NY, USA.
Neuropharmacology. 2019 Nov 1;158:107619. doi: 10.1016/j.neuropharm.2019.04.025. Epub 2019 Apr 25.
Pain remains a global health challenge. For decades, clinicians have been primarily relying on μ-opioid receptor (MOR) agonists and nonsteroidal anti-inflammatory drugs (NSAIDs) for pain management. MOR agonists remain the most efficacious analgesics available; however, adverse effects related to MOR agonists use are severe which often lead to forced drug discontinuation and inadequate pain relief. The recent opioid overdose epidemic urges the development of safer analgesics. Combination therapy is a well-established clinical pharmacotherapeutic strategy for the treatment of various clinical disorders. The combination of MOR agonists with non-MOR agonists may increase the analgesic potency of MOR agonists, reduce the development of tolerance and dependence, reduce the diversion and abuse, overdose, and reduce other clinically significant side effects associated with prolonged opioid use such as constipation. Overall, the combination therapy approach could substantially improve the therapeutic profile of MOR agonists. This review summarizes some recent developments in this field. This article is part of the Special Issue entitled 'New Vistas in Opioid Pharmacology'.
疼痛仍然是一个全球性的健康挑战。几十年来，临床医生主要依赖 μ 阿片受体（MOR）激动剂和非甾体抗炎药（NSAIDs）来进行疼痛管理。MOR 激动剂仍然是最有效的镇痛药；然而，与 MOR 激动剂使用相关的不良反应非常严重，这往往导致被迫停药和疼痛缓解不足。最近的阿片类药物过量流行促使开发更安全的镇痛药。联合治疗是治疗各种临床疾病的一种成熟的临床药物治疗策略。MOR 激动剂与非 MOR 激动剂的联合使用可能会增加 MOR 激动剂的镇痛效力，减少耐受性和依赖性的发展，减少滥用、过量和与长期使用阿片类药物相关的其他临床上显著的副作用，如便秘。总的来说，联合治疗方法可以显著改善 MOR 激动剂的治疗效果。本综述总结了该领域的一些最新进展。本文是“阿片类药物药理学的新视角”特刊的一部分。
